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Multiparticulate Enteric Coated Formulation of Chloroquine Phosphate for Better Patient Compliance

Author(s): Brinda Sreelesh, J. G. Avari, Manju Nagpal, Pankaj Rakha and Gitika Dhingra

Chloroquine is an excellent antimalarial as well as an antiamoebic drug. It is the first drug of choice in the treatment of malaria. Chloroquine is a highly bitter drug and the oral marketed tablet has serious distressing side effects like gastrointestinal irritation leading to nausea, vomiting and diarrhea. In the present study, an enteric coated formulation of chloroquine phosphate was prepared using Acrycoat L- 100. Pellets of chloroquine phosphate were prepared using different concentrations of Acrycoat L-100, the enteric coating polymer and dibutyl phthalate (DBP) as plasticizer. The prepared pellets were evaluated for their flow properties, friability, true density, bulk density, SEM studies, content uniformity and in vitro release studies. The physical parameters were observed to give excellent flow properties. The spherical shape and coating uniformity was indicated in the scanning electron micrographs. The in vitro dissolution studies revealed that formulation batch A6 (10% Acrycoat L-100 and 30% of DBP) as the best batch out of A1-A6 batches as it showed a release of less than 9 % in the acidic medium and more than 80 % in the basic medium in 45 min. resulting in improved bioavailability and patient compliance.

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